Synthesis and some pharmacological studies of new benzenesulfonamide derivatives

New benzenesulfonamide derivatives containing pyrazole and oxadiazole moieties were prepared starting from sodium saccharin. The structures of the novel compounds were characterized by elemental analyses and spectroscopic methods. The new compounds are structurally related to the COX-2 inhibitor celecoxib (Celebrex(R)). A pharmacological study of the pyrazoles revealed that several compounds possess higher analgesic and antiinflammatory activities than celecoxib, particularly 11 and 17. Most of the pyrazoles showed a significant increase in the sleeping time of thiopentone anaesthesized mice and also protected mice against the convulsive and lethal effects of Pentylenetetrazole. Moreover, the ulcerogenic activity of those compounds showing a pronounced antiinflammatory effect was also studied.